CXCR4 chemokine receptors, are found on the surface of immune cells, and interact with the specific natural ligand, known as CXCL12 or stromal cell-derived factor 1α (SDF-1α). They have been revealed to play a role in a number of disease states. For example the CXCR4 SDF-1α system has involvement in cancer progression and metastasis, and in the development of rheumatoid arthritis. CXCR4 and CCR5 co-receptors have been identified as the entry route for HIV into cells, providing a new therapeutic approach to treatment by entry inhibitor drugs rather than the current preference for reverse transcriptase and protease inhibitors. An object of the present invention is to provide new antagonists for the CXCR4 co-receptor.
This invention may provide novel compounds that selectively bind to chemokine receptors based on cross bridged macrocycles. The compounds may incorporate metal ions and form stable complexes prior to administration.
It is an object of this invention to provide examples of bridged azamacrocyclic derivatives that show specific chemokine receptor binding.